Name | GNE-9605 |
Description | GNE-9605 is a highly effective, specifical, and brain-penetrant LRRK2 inhibitor (IC50: 19 nM). |
In vitro | In rats, PKGNE-9605 administered orally at a dose of 1 mg/kg exhibited a total plasma clearance rate of 26 mL/min/kg, achieving an oral bioavailability of 90%. In BAC transgenic mice models expressing the human LRRK2 G2019S mutation associated with Parkinson's disease, GNE-9605, administered intraperitoneally at doses of 10 and 50 mg/kg, was able to inhibit the autophosphorylation of LRRK2 at Ser1292. |
In vivo | In vitro human MDR1 permeability data indicate that GNE-9605 exhibits favorable brain penetration in higher organisms. In biochemical (Ki: 2.0 nM) and cellular (IC50: 19 nM) assays, GNE-9605 demonstrates potent inhibitory activity against LRRK2. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 82 mg/mL (182.3 mM) Ethanol : 10 mg/mL (22.2 mM)
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Keywords | oral bioavailability | Leucine-rich repeat kinase 2 | GNE-9605 | Parkinson's disease | LRRK2 Ser1292 | GNE 9605 | autophosphorylation | Inhibitor | LRRK2 | GNE9605 | inhibit |
Inhibitors Related | PFE-360 | GNE0877 | CZC-25146 | GSK2578215A | CZC-54252 hydrochloride | GNE-7915 | EB-42486 | LRRK2 inhibitor 1 | LRRK2-IN-7 | LRRK2-IN-1 | CCG-1423 | PF-06454589 |
Related Compound Libraries | Target-Focused Phenotypic Screening Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Autophagy Compound Library | CNS-Penetrant Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Fluorochemical Library |